Technetium-99m labeling of N-[N-(3-diphenylphosphino propionyl)glycyl]cysteine (PN2S-OH) and its methyl ester derivative (PN2S-OMe)

Nucl Med Biol. 2004 Jul;31(5):655-62. doi: 10.1016/j.nucmedbio.2004.02.001.

Abstract

N-[N-(3-diphenylphosphinopropionyl)glycyl]cysteine and its methyl ester derivative were labeled with (99m)Tc at neutral pH, leading to a single species in high yield (>95%) in 30 min. RP-HPLC comparison with the analogue Re(V)-oxo complexes identified the labeled compounds as the anti isomers of pentacoordinated (99m)TcO[PN(2)S]-OH and (99m)TcO[PN(2)S]-OMe complexes. The compounds are stable from pH 7 to pH 9 when (99m)TcO[PN(2)S]-OH interconverts to related syn isomer, while (99m)TcO[PN(2)S]-OMe undergoes both saponification and interconversion. They exhibit high stability in human plasma and in vivo (mice), and a biodistribution characterized by hepatobiliary excretion.

Publication types

  • Comparative Study
  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dipeptides / blood
  • Dipeptides / pharmacokinetics*
  • Humans
  • Isotope Labeling / methods
  • Liver / diagnostic imaging*
  • Liver / metabolism*
  • Male
  • Metabolic Clearance Rate
  • Mice
  • Organ Specificity
  • Organotechnetium Compounds / blood
  • Organotechnetium Compounds / pharmacokinetics*
  • Radionuclide Imaging
  • Radiopharmaceuticals / blood
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Tissue Distribution

Substances

  • Dipeptides
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • technetium 99m N-(N-(3-diphenylphosphinopropionyl)glycyl)cysteine
  • technetium 99m N-(N-(3-diphenylphosphinopropionyl)glycyl)cysteine methyl ester